There are numerous 5-HT.sub.1A receptor inhibitors that are known. However, none that are currently known are selective. In other words, those that are known are often also blockers for other receptors such as dopamine, norepinephrine, and/or acetyl choline. None that are presently known are selective only for serotonin 5-HT.sub.1A receptor blocking.
Of course, it is highly desirable to have compounds which function very specifically for blocking of serotonin receptors since that would allow highly specific effects, without causing undesirable side effects.
Some of the potential uses that may exist for a highly specific serotonin 5-HT.sub.1A receptor blocker would include potential use as an antidote for counteracting the effects of cocaine and for an effective appetite suppressant.
An earlier paper by some of the present inventors has reported that R-11-hydroxy-10-methylaporphine is in fact an agonist for 5-HT.sub.1A receptors. It is highly surprising that the (S)-enantiomer shows no agonist effect, but in fact blocks the action of serotonin 5-HT.sub.1A receptors. This is a rare example of enantiomers which demonstrate exactly opposite pharmacological effects at the same receptor.
A primary objective of the present invention is to make S-11-hydroxy-10-methylaporphine and its biologically active salt forms.
Another objective of the present invention is to develop a method of selective inhibition of serotonin 5-HT.sub.1A receptors in mammals by administering S-11-hydroxy-10-methylaporphine or a biologically acceptable salt form thereof.
Another objective of the present invention is to provide compositions containing S-11-hydroxy-10-methylaporphine or a biologically acceptable salt form thereof which can be effectively used for an antidote for the effects of cocaine and/or for use as an appetite suppressant.
The method of accomplishing these as well as other objectives of the present invention will become apparent from the detailed description of the invention which will follow hereinafter.